Journal
MOLECULES
Volume 13, Issue 4, Pages 736-748Publisher
MDPI
DOI: 10.3390/molecules13040736
Keywords
hyaluronidase; benzimidazole; benzothiazole; indole; Morgan-Elson assay; stains-all assay and microwave irradiation
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We have synthesized twelve 2-substituted benzimidazole, benzothiazole and indole derivatives using on both microwave irradiation and conventional heating methods. The microwave method was observed to be more beneficial as it provides an increase of yield from 3% to 113% and a 95 to 98% reduction in time. All compounds were tested by a stains-all assay at pH 7 and by a Morgan-Elson assay at pH 3.5 for hyaluronidase inhibitory activity at a concentration of 100 mu M. The most potent compound was 2-(4-hydroxyphenyl)-3-phenylindole (12) with an IC50 value of 107 mu M at both pH 7 and 3.5.
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